YIL781 hydrochloride is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 hydrochloride produces a greater improvement in glucose homeostasis in rats. YIL-781 hydrochloride inhibits the calcium response induced by ghrelin with pIC 50 values of 7.90 and 8.27, respectively.
性状
Solid
体外研究(In Vitro)
YIL-781 (10-300 nM) induces a concentration-dependent parallel rightward shift of the ghrelin CRC with a slight but statistically significant depression of the maximal response at 100 and 300 nM, reaching a similar agonist maximal response of approximately 90%. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
YIL781 (0.1 to 5 μg/5 μl) attenuates ghrelin-induced up-regulation of the blood glucose level. The
i.t. treatment with YIL781 alone does not affect the blood glucose level (F = 0.8160; P = 0.5095). has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. William P Esler, et al. Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss Endocrinology. 2007 Nov;148(11):5175-85.[2]. Timothy H. Moran, et al. Gut Peptides: Targets for Antiobesity Drug Development? Endocrinology. 2009 Jun; 150(6): 2526–2530.
[1]. William P Esler, et al. Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss Endocrinology. 2007 Nov;148(11):5175-85.[2]. Timothy H. Moran, et al. Gut Peptides: Targets for Antiobesity Drug Development? Endocrinology. 2009 Jun; 150(6): 2526–2530.